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Quinoline carboxamide-type ABCG2 modulators: Indole and quinoline moieties as anilide replacements

Bauer, Stefanie, Ochoa Puentes, Cristian, Sun, Qiu, Bause, Manuel, Bernhardt, Günther, König, Burkhard and Buschauer, Armin (2013) Quinoline carboxamide-type ABCG2 modulators: Indole and quinoline moieties as anilide replacements. ChemMedChem 8 (11), pp. 1773-1778.

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Abstract

Bioisosteric replacement of the anilide core by an indole moiety considerably increased stability and gave potent and selective ABCG2 (BCRP) inhibitors. Some compounds are superior to the reference substances fumitremorgin C and Ko143 in terms of potency and efficacy and are the most potent ABCG2 modulators reported so far.


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Item type:Article
Date:28 August 2013
Additional Information (public):Umfangreiche Supporting Information (81 Seiten)
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Identification Number:
ValueType
10.1002/cmdc.201300319DOI
24039190PubMed ID
Related URLs:
URLURL Type
http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201300319/fullPublisher
http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201300319/suppinfoSupplementary Material
Keywords:ABCB1, ABCG2, ABC transporter, breast cancer resistance protein, Inhibitors, Sonogashira coupling, Synthesis, UR COP269
Dewey Decimal Classification:500 Science > 540 Chemistry & allied sciences
600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:28575
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